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A kind of loratadine nano crystal and preparation method thereof

A loratadine and nanocrystal technology, which is applied in the field of pharmaceutical nanocrystals and their preparation, can solve the problems of difficulty in process control, generation of organic solvents, difficulty in large-scale production, etc., and achieves controllable preparation process and reduced energy consumption for homogenization. , the effect of narrow distribution

Active Publication Date: 2022-02-11
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention adopts high-speed shearing combined with high-pressure homogenization technology to prepare loratadine into drug nanocrystals. Compared with other nanocrystal preparation technologies, this technology has obvious advantages. Chinese patent CN 110354075 A discloses a solvent precipitation method to prepare chloratadine The method of Ratadine nano-suspension, but this method has problems such as producing organic solvent, having solvent residue, process control difficulty, being difficult to industrialized large-scale production

Method used

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  • A kind of loratadine nano crystal and preparation method thereof
  • A kind of loratadine nano crystal and preparation method thereof
  • A kind of loratadine nano crystal and preparation method thereof

Examples

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Effect test

Embodiment 1

[0036] Weigh 1 part of Tween 80 and add it into 20ml of pure water, place it on a magnetic stirrer at 200rpm and stir until completely dissolved, weigh 5 parts of loratadine raw material, add the aqueous solution containing Tween 80 under stirring During the process, the stirring was continued for 5 minutes to disperse the loratadine in the aqueous stabilizer solution, and the high-speed shear was cut at 1000 rpm for 1 minute to obtain a coarse suspension. Pour the coarse suspension into the feed port of the high-pressure homogenizer, circulate 10 times at 400 bar, and then circulate 10 times at 1000 bar to obtain the loratadine suspension. Add lactose into the prepared loratadine nanosuspension, shake it to fully dissolve, place it in a refrigerator at -80°C for 12 hours, and then freeze it in a freeze dryer for 48 hours to obtain a plump and loose chloratadine. Ratadine nano crystals, the prepared loratadine nano crystals have a particle size of 758.4nm and a PDI of 0.248. ...

Embodiment 2

[0038] Weigh 20 parts of Poloxamer 188 and add it into 20ml of pure water, place it on a magnetic stirrer and stir at 1000rpm until completely dissolved, weigh 50 parts of loratadine raw material, add the poloxamer containing poloxamer under stirring In the aqueous solution of M188, continue to stir for 15 minutes to disperse loratadine in the aqueous solution of the stabilizer, and shear at 6000 rpm for 15 minutes with a high-speed shearer to obtain a coarse suspension. Pour the coarse suspension into the feed port of the high-pressure homogenizer, circulate 30 times at 1000 bar, and circulate 50 times at 2400 bar to obtain the loratadine suspension. Add lactose into the prepared loratadine nanosuspension, shake it to fully dissolve, place it in a refrigerator at -80°C for 12 hours, and then freeze it in a freeze dryer for 48 hours to obtain a plump and loose chloratadine. Ratadine nano crystals, the prepared loratadine nano crystals have a particle size of 593.2nm and a PDI ...

Embodiment 3

[0040]Weigh 20 parts of Poloxamer 188 and add it into 20ml of pure water, place it on a magnetic stirrer and stir at 1000rpm until completely dissolved, weigh 50 parts of loratadine raw material, add the poloxamer containing poloxamer under stirring In the aqueous solution of M188, continue to stir for 15 minutes to disperse loratadine in the aqueous solution of the stabilizer, and shear at 6000 rpm for 15 minutes with a high-speed shearer to obtain a coarse suspension. Pour the coarse suspension into the feed port of the high-pressure homogenizer, circulate 30 times at 600 bar, and circulate 50 times at 2200 bar to obtain the loratadine suspension. Add lactose into the prepared loratadine nanosuspension, shake it to fully dissolve, place it in a refrigerator at -80°C for 12 hours, and then freeze it in a freeze dryer for 48 hours to obtain a plump and loose chloratadine. Ratadine nano crystals, the prepared loratadine nano crystals have a particle size of 412.7nm and a PDI of...

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Abstract

The invention belongs to the field of pharmaceutical preparations and discloses a preparation method of loratadine nano crystals and oral tablets thereof. Loratadine is a kind of BCS Ⅱ medicine, and its solubility is extremely low and is pH-dependent. In order to improve the dissolution rate and bioavailability of the medicine and improve individual variability, the present invention adopts high-speed shearing combined with high-pressure homogenization method to prepare loratadine. The radadine nano crystal adopts the powder direct compression method to prepare the loratadine nano crystal oral tablet. The preparation process of the invention is simple, fast, environment-friendly and easy for industrialized large-scale production. The dissolution rate was evaluated by an in vitro dissolution test. The loratadine nanocrystals and tablets prepared by this method can be rapidly dissolved in various pH media, thereby improving bioavailability and improving individual variability.

Description

technical field [0001] The invention relates to a drug nanocrystal and a preparation method thereof, in particular to a loratadine nanocrystal and a preparation method thereof. Background technique [0002] The chemical name of loratadine is 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-6]pyridin-11-ylidene) -l-piperidinecarboxylic acid ethyl ester (structural formula is as follows), molecular formula C 22 h 23 C l N 20 , molecular weight: 382.89. [0003] [0004] Loratadine is a second-generation histamine H1 receptor antagonist and is the most commonly used antihistamine in the clinical treatment of allergic diseases (such as rhinitis, urticaria and atopic dermatitis). Loratadine is easily soluble in organic solvents such as methanol, ethanol, and chloroform, and is almost insoluble in water (about 3 μg / ml), but has high permeability (logP=5). Loratadine is a weakly basic compound, and its solubility It is pH dependent, and its solubility decreases signifi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K9/20A61K47/26A61K47/10A61K31/4545A61P37/08
CPCA61K9/19A61K9/2031A61K31/4545A61P37/08
Inventor 孙敏捷李菁玛依努尔·艾沙周颖平
Owner CHINA PHARM UNIV
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